Majumdar S S, Chaudhary J, Sharma R K, Das R P
Department of Reproductive Biomedicine, National Institute of Health and Family Welfare, Munirka, New Delhi, India.
Contraception. 1990 Jun;41(6):641-53. doi: 10.1016/s0010-7824(09)91009-5.
STS-557 (17 alpha-cyanomethyl-17 beta-hydroxy-estra-4, 9(10)-diene-3-one) was administered (i.m.) to two groups (4 in each group) of adult male bonnet monkeys at a daily dose of 10 mg/monkey for 12 weeks (first group) and 5 mg/monkey for 14 weeks (second group). Treatment with the 10 mg dose resulted in a significant decline in the count, motility, acrosin and hyaluronidase activities and the fertilizing ability (zona-free hamster egg penetration assay) of spermatozoa by the 6th week of initiation of treatment. The circulating level of STS-557 was low after one week and increased from the 2nd week of treatment when the serum level of testosterone was significantly reduced. Complete recovery was observed by the 11th week after withdrawal of treatment. The treatment with the 5 mg dose had minor and inconsistent effect on the motility, hyaluronidase and acrosin activity, and the fertilizing ability of spermatozoa in addition to the blood level of testosterone. STS-557 may have the potentiality to be used as a chemical contraceptive in the male but compensation for the reduced level of blood testosterone may be necessary.
将STS - 557(17α - 氰甲基 - 17β - 羟基 - 雌甾 - 4,9(10) - 二烯 - 3 - 酮)以肌肉注射的方式给予两组成年雄性冠毛猕猴(每组4只),第一组每日剂量为10毫克/只,持续12周;第二组每日剂量为5毫克/只,持续14周。用10毫克剂量治疗时,在治疗开始后的第6周,精子的数量、活力、顶体蛋白酶和透明质酸酶活性以及受精能力(无透明带仓鼠卵穿透试验)显著下降。治疗1周后,STS - 557的循环水平较低,从治疗第2周开始升高,此时睾酮的血清水平显著降低。停药后第11周观察到完全恢复。除了睾酮的血液水平外,5毫克剂量的治疗对精子活力、透明质酸酶和顶体蛋白酶活性以及受精能力有轻微且不一致的影响。STS - 557可能有潜力用作男性化学避孕药,但可能需要补偿血液中睾酮水平的降低。